诺氟沙星 | 70458-96-7

• 物质功能分类: 原料药 - 人工合成抗感染类药 - 喹诺酮类药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 诺氟沙星
• 中文别名: 氟哌酸；1-乙基-6-氟-1,4-二氢-4-氧代-7-(1-哌嗪基)-3-喹啉羧酸
• 英文名称: 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid
• 英文别名: norfloxacin；norfloxacine；NFX；1-ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid；NOR；1-Ethyl-6-fluoro-4-oxo-7-piperazin-4-ium-1-ylquinoline-3-carboxylate
• CAS: 70458-96-7
• 化学式: C₁₆H₁₈FN₃O₃
• mdl: MFCD00079532
• 分子量: 319.336
• InChiKey: OGJPXUAPXNRGGI-UHFFFAOYSA-N

物化性质

• 熔点：
  220°C
• 沸点：
  555.8±50.0 °C(Predicted)
• 密度：
  1.2504 (estimate)
• 溶解度：
  极微溶于水，微溶于丙酮和乙醇（96%）。
• 物理描述：
  Solid
• 颜色/状态：
  White to light-yellow crystalline powder
• 分解：
  When heated to decompostion it emits toxic fumes of /hydrogen fluoride and nitrogen oxides/.
• 解离常数：
  pKa1 = 6.34; pKa2 = 8.75
• 碰撞截面：
  184.2 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]
• 稳定性/保质期：
  在常温常压下保持稳定，请远离氧化剂。

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.375
• 拓扑面积：
  72.9
• 氢给体数：
  2
• 氢受体数：
  7

ADMET

代谢

经肝和肾

Via liver and kidney

来源:DrugBank

代谢

诺氟沙星通过肾脏和非肾脏机制消除。该药物部分通过改变哌嗪基团代谢为6种代谢物，分别命名为M-1、M-2、M-3、M-4(1)、M-4(2)和M-5。2虽然其中一些代谢物在微生物学上具有活性，但它们比母药活性弱。有人提出诺氟沙星在肝脏经历首过代谢，但需要进一步研究以充分阐明药物的代谢命运。

Norfloxacin is eliminated by renal and nonrenal mechanisms. The drug is partially metabolized by modification of the piperazinyl group to 6 metabolites, designated M-1, M-2, M-3, M-4(1), M-4(2), and M-5.2 Although some of the metabolites are microbiologically active, they are less active than the parent drug. It has been suggested that norfloxacin undergoes first-pass metabolism in the liver, but further study is needed to fully elucidate the metabolic fate of the drug.

来源:Hazardous Substances Data Bank (HSDB)

代谢

培氟沙星，N-去甲基是培氟沙星的人类已知代谢物。

Pefloxacin, N-desmethyl is a known human metabolite of Pefloxacin.

来源:NORMAN Suspect List Exchange

毒理性

• 肝毒性

诺氟沙星与其他氟喹诺酮类药物一样，在治疗期间与低比率的血清酶升高（1%至3%）有关。这些异常通常是轻微的、无症状的，并且是暂时的，即使在继续治疗的情况下也会解决。诺氟沙星还与罕见但偶尔严重甚至致命的急性肝损伤病例有关。尽管病例数量很少，但临床模式一直是一致的，潜伏期短，为1天至3周，肝细胞损伤突然发作。血清酶升高的模式可以是肝细胞性或胆汁淤积性，发病时间较短的病例通常更倾向于肝细胞性，ALT水平显著升高，偶尔伴有凝血酶原时间的快速恶化和肝功能衰竭的迹象。疾病发作可能在停药后几天内发生。许多（但并非所有）病例出现了过敏表现，如发热、皮疹和嗜酸性粒细胞增多。自身抗体通常不存在。还描述了胆汁淤积性和混合性损伤模式，特别是在肝损伤被延迟识别的情况下。这些特征是所有与氟喹诺酮类药物相关的肝毒性的典型表现，认为这种损伤是特定于类药物的。

Norfloxacin like other fluoroquinolones is associated with a low rate (1% to 3%) of serum enzyme elevations during therapy. These abnormalities are generally mild, asymptomatic and transient, resolving even with continuation of therapy. Norfloxacin has also been linked to rare but occasionally severe and even fatal cases of acute liver injury. While the numbers of cases have been few, the clinical pattern has been consistent with short latency period of 1 day to 3 weeks and abrupt onset of hepatocellular injury. The pattern of serum enzyme elevations can be either hepatocellular or cholestatic, cases with the shorter times to onset usually being more hepatocellular with markedly elevated ALT levels, and occasionally with rapid worsening of prothrombin time and signs of hepatic failure. The onset of illness may occur a few days after the medication is stopped. Many (but not all) cases have had allergic manifestations with fever, rash and eosinophilia. Autoantibodies are usually not present. Cholestatic and mixed patterns of injury have also been described particularly with delayed recognition of the liver injury. These features are typical of all fluoroquinolone associated hepatotoxicity and the injury is believed to be class specific.

来源:LiverTox

毒理性

• 药物性肝损伤

化合物：诺氟沙星

Compound:norfloxacin

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注解：较少的药物性肝损伤关注

DILI Annotation:Less-DILI-Concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

严重性等级：3

Severity Grade:3

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：警告和预防措施

Label Section:Warnings and precautions

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

• 吸收

快速

Rapid

来源:DrugBank

吸收、分配和排泄

• 消除途径

诺氟沙星通过代谢、胆汁排泄和肾脏排泄被消除。在肾脏排泄过程中，预计它将经历肾小球滤过和肾小管分泌，其高肾脏清除率约为275 mL/min就证明了这一点。

Norfloxacin is eliminated through metabolism, biliary excretion, and renal excretion. It is expected to undergo both glomerular filtration and tubular secretion during renal excretion, as shown by its high renal clearance rate of approximately 275 mL/min.

来源:DrugBank

吸收、分配和排泄

Norfloxacin crosses the placenta and is distributed into cord blood and amniotic fluid. It is not known whether the drug is distributed into milk. Norfloxacin was not detected in the milk of lactating women following a single 200-mg oral dose of the drug, but the possibility of distribution into milk following higher doses remains to be determined. Some other quinolones (e.g., ciprofloxacin, levofloxacin ofloxacin) are distributed into milk. 诺氟沙星可穿过胎盘并分布到脐带血和羊水中。目前尚不清楚该药物是否分布到乳汁中。在给予哺乳妇女单次200毫克口服剂量后，未在乳汁中检测到诺氟沙星，但在更高剂量后药物分布到乳汁中的可能性仍有待确定。其他一些喹诺酮类药物（例如，环丙沙星、左氧氟沙星、氧氟沙星）会分布到乳汁中。

Norfloxacin crosses the placenta and is distributed into cord blood and amniotic fluid. It is not known whether the drug is distributed into milk. Norfloxacin was not detected in the milk of lactating women following a single 200-mg oral dose of the drug, but the possibility of distribution into milk following higher doses remains to be determined. Some other quinolones (e.g., ciprofloxacin, levofloxacin ofloxacin) are distributed into milk.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在成年人中，那些每天两次口服400毫克诺氟沙星的患者，获得的药物在前列腺组织中的浓度范围在第二次给药后1-4小时内取得的标本中为0.24-4.65微克/克；同时血清中的药物浓度范围在0.42-5.3微克/毫升。诺氟沙星与血清蛋白的结合率为10-15%。

In adults who received 400 mg of oral norfloxacin twice daily, prostatic tissue concentrations of the drug ranged from 0.24-4.65 ug/g in specimens obtained 1-4 hours after the second dose; concurrent serum concentrations ranged from 0.42-5.3 ug/mL. Norfloxacin is 10-15% bound to serum proteins.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

胆汁中诺氟沙星的浓度可能比同时期的血清浓度高出10倍。在接受胆囊切除术的患者中，术前单次口服400毫克诺氟沙星后，药物浓度在胆汁中为0.6-15.6微克/毫升，在胆囊组织中为0.4-7.5微克/克，在大约服药后3.5-6小时取得的血清样本中为0.4-1.8微克/毫升。

Biliary concentrations of norfloxacin may be up to 10 times higher than concurrent serum concentrations. In cholecystectomy patients who received a single 400-mg oral dose of norfloxacin prior to surgery, concentrations of the drug ranged from 0.6-15.6 ug/mL in gallbladder bile, from 0.4-7.5 mcg/g in gallbladder tissue, and from 0.4-1.8 ug/mL in serum in specimens obtained approximately 3.5-6 hours after the dose.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xn
• 安全说明：
  S26,S37/39
• 危险类别码：
  R20/21/22
• WGK Germany：
  2
• 海关编码：
  2933990090
• 危险品运输编号：
  NONH for all modes of transport
• RTECS号：
  VB2005000
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335
• 储存条件：
  存放在密封容器中，并置于阴凉、干燥处，建议在2-8 ºC条件下保存。

SDS

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Section I.Chemical Product and Company Identification
Chemical Name Norfloxacin
Portland OR
Synonym 3-Quinolinecarboxylic acid, 1-ethyl-6-fluoro-1,4-
dihydro-4-oxo-7-(1-piperazinyl)- (CA INDEX NAME);
1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-
3-quinolinecarboxylic Acid
Chemical Formula C16H18FN3O3
CAS Number 70458-96-7

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Section II. Composition and Information on Ingredients
Toxicology Data
Chemical Name CAS Number Percent (%) TLV/PEL
Min. 98.0 Not available. Rat LD50 (oral) >4 gm/kg
Norfloxacin 70458-96-7
(HPLC,T) Mouse LD50 (intraperitoneal) 1064
mg/kg
Rat LD50 (intravenous) 245 mg/kg

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Section III. Hazards Identification
No specific information is available in our data base regarding the toxic effects of this material for humans. However,
Acute Health Effects
exposure to any chemical should be kept to a minimum. Skin and eye contact may result in irritation. May be harmful if
inhaled or ingested. Always follow safe industrial hygiene practices and wear proper protective equipment when handling
this compound.
CARCINOGENIC EFFECTS : Not available.
Chronic Health Effects
MUTAGENIC EFFECTS : Not available.
TERATOGENIC EFFECTS : Not available.
DEVELOPMENTAL TOXICITY: Reproductive effects.
Rat TDLo Oral 1375 mg/kg, female 7-17 days of pregnancy
Toxic Effects:
Specific Developmental Abnormalities - Musculoskeletal system
Effects on Newborn - Behavioral
Rabbit Oral 1300 mg/kg, female 6-18 days of pregnancy
Toxic Effects:
Effects on Fertility - Litter size
Effects on Embryo or Fetus - Fetotoxicity
Effects on Embryo or Fetus - Fetal death
Rabbit Oral 1625 mg/kg, female 13 days prior to mating
Toxic Effects:
Maternal Effects - Ovaries, fallopian tubes
Maternal Effects - Uterus, cervix, vagina
Repeated or prolonged exposure to this compound is not known to aggravate existing medical conditions.

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Section IV. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at least 15
minutes. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Remove contaminated clothing and shoes. Wash clothing
before reuse. Thoroughly clean shoes before reuse. Get medical attention.
Inhalation If the victim is not breathing, perform mouth-to-mouth resuscitation. Loosen tight clothing such as a collar, tie, belt or
waistband. If breathing is difficult, oxygen can be administered. Seek medical attention if respiration problems do not
improve.
INDUCE VOMITING by sticking finger in throat. Lower the head so that the vomit will not reenter the mouth and throat.
Ingestion
Loosen tight clothing such as a collar, tie, belt or waistband. If the victim is not breathing, perform mouth-to-mouth
resuscitation. Examine the lips and mouth to ascertain whether the tissues are damaged, a possible indication that the toxic
material was ingested; the absence of such signs, however, is not conclusive.
Continued on Next Page
Norfloxacin

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Section V. Fire and Explosion Data
Not available.
Flammability May be combustible at high temperature. Auto-Ignition
Flammable Limits Not available.
Flash Points Not available.
Combustion Products These products are toxic carbon oxides (CO, CO2), nitrogen oxides (NO, NO2), halogenated compounds.
WARNING: Highly toxic HF gas is produced during combustion.
Fire Hazards Not available.
Risks of explosion of the product in presence of mechanical impact: Not available.
Explosion Hazards
Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media
SMALL FIRE: Use DRY chemical powder.
LARGE FIRE: Use water spray, fog or foam. DO NOT use water jet.
and Instructions
Consult with local fire authorities before attempting large scale fire-fighting operations.

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Section VI. Accidental Release Measures
Spill Cleanup Hygroscopic material.
Use a shovel to put the material into a convenient waste disposal container. Finish cleaning the spill by rinsing any
Instructions
contaminated surfaces with copious amounts of water. Consult federal, state, and/or local authorities for assistance on
disposal.

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Section VII. Handling and Storage
HYGROSCOPIC. Keep away from heat. Mechanical exhaust required. When not in use, tightly seal the container and store
Handling and Storage
in a dry, cool place. Avoid excessive heat and light. Do not breathe dust.
Information
Always store away from incompatible compounds such as oxidizing agents, moisture.

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Section VIII. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below recommended
exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to airborne contaminants
below the exposure limit.
Personal Protection Splash goggles. Lab coat. Dust respirator. Boots. Gloves. Suggested protective clothing might not be sufficient; consult a
specialist BEFORE handling this product. Be sure to use a MSHA/NIOSH approved respirator or equivalent.
Not available.
Exposure Limits

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Section IX. Physical and Chemical Properties
Physical state @ 20°C Solid. (Very pale yellow ~ pale yellow, Solubility Solubility at 25°C (mg/ml): water 0.28;
crystal ~ powder.)
methanol 0.98; ethanol 1.9; acetone 5.1;
chloroform 5.5; diethyl ether 0.1; benzene
Not available.
Specific Gravity
0.15; ethyl acetate 0.94; octyl alcohol 5.1;
glacial acetic acid 340.
Solubility in water is pH dependent,
increasing sharply at pH <5 or at pH >10.
Molecular Weight 319.33 Partition Coefficient LOG Pow: 0.46
Boiling Point Not available. Not applicable.
Vapor Pressure
Melting Point 221°C (429.8°F) Vapor Density Not available.
Not available. Not available.
Refractive Index Volatility
Critical Temperature Not available. Odor Not available.
Not available. Not available.
Viscosity Taste

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Section X. Stability and Reactivity Data

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This material is stable if stored under proper conditions. (See Section VII for instructions)
Stability
Conditions of Instability Avoid excessive heat and light. Hygroscopic; keep container tightly closed.
Incompatibilities Reactive with oxidizing agents, moisture.
Continued on Next Page
Norfloxacin

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Section XI. Toxicological Information
RTECS Number VB2005000
Eye Contact. Ingestion. Inhalation.
Routes of Exposure
Toxicity Data Rat LD50 (oral) >4 gm/kg
Mouse LD50 (intraperitoneal) 1064 mg/kg
Rat LD50 (intravenous) 245 mg/kg
Chronic Toxic Effects CARCINOGENIC EFFECTS : Not available.
MUTAGENIC EFFECTS : Not available.
TERATOGENIC EFFECTS : Not available.
DEVELOPMENTAL TOXICITY: Reproductive effects.
Rat TDLo Oral 1375 mg/kg, female 7-17 days of pregnancy
Toxic Effects:
Specific Developmental Abnormalities - Musculoskeletal system
Effects on Newborn - Behavioral
Rabbit Oral 1300 mg/kg, female 6-18 days of pregnancy
Toxic Effects:
Effects on Fertility - Litter size
Effects on Embryo or Fetus - Fetotoxicity
Effects on Embryo or Fetus - Fetal death
Rabbit Oral 1625 mg/kg, female 13 days prior to mating
Toxic Effects:
Maternal Effects - Ovaries, fallopian tubes
Maternal Effects - Uterus, cervix, vagina
Repeated or prolonged exposure to this compound is not known to aggravate existing medical conditions.
Acute Toxic Effects No specific information is available in our data base regarding the toxic effects of this material for humans. However,
exposure to any chemical should be kept to a minimum. Skin and eye contact may result in irritation. May be harmful if
inhaled or ingested. Always follow safe industrial hygiene practices and wear proper protective equipment when handling this
compound.

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Section XII. Ecological Information
Not available.
Ecotoxicity
Not available.
Environmental Fate

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Section XIII. Disposal Considerations
Waste Disposal Recycle to process, if possible. Consult your local regional authorities. You may be able to dissolve or mix material with a
combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber system. Observe all
federal, state and local regulations when disposing of the substance.

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Section XIV. Transport Information
DOT Classification Not a DOT controlled material (United States).
PIN Number Not applicable.
Proper Shipping Name Not applicable.
Packing Group (PG) Not applicable.
DOT Pictograms

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Section XV. Other Regulatory Information and Pictograms
TSCA Chemical Inventory This product is NOT on the EPA Toxic Substances Control Act (TSCA) inventory. The following notices are required by 40
CFR 720.36 (C) for those products not on the inventory list:
(EPA)
(i) These products are supplied solely for use in research and development by or under the supervision of a technically
qualified individual as defined in 40 CFR 720.0 et sec.
(ii) The health risks of these products have not been fully determined. Any information that is or becomes available will be
supplied on an MSDS sheet.
WHMIS Classification On DSL.
(Canada)
EINECS Number (EEC) 274-614-4
EEC Risk Statements Not available.
Japanese Regulatory Data Not available.
Continued on Next Page

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

诺氟沙星是一种第三代喹诺酮类抗菌药物，具有广谱高效的抗菌作用。以下是其详细信息：

用途

1. 尿路感染：用于治疗由敏感细菌引起的泌尿系统感染。
2. 淋病：有效对抗淋球菌引起的各种感染。
3. 前列腺炎：对于前列腺炎症有一定的疗效。
4. 肠道感染：适用于大肠杆菌、沙门氏菌等导致的肠道感染。
5. 外科和妇科感染：对这些部位的一些细菌感染有效。
6. 五官科感染：用于治疗眼部、耳部等部位由敏感细菌引起的感染。
7. 皮肤科感染：可用于一些皮肤感染性疾病。

化学性质

• 化学名称：7-氟-6-氧代-1-哌嗪基-3-(1H)-喹啉甲酸乙酯
• 分子式：C16H18FN3O3
• 分子量：319.34

物理性质

• 熔点：220-221℃
• UV吸收峰：λmax 274, 325, 336 nm (ε≈1109, 437, 425)

生产方法

1. 首先从邻二氯苯或对硝基氯苯出发，经过硝化、氟化等步骤制得3-氯-4-氟硝基苯。
2. 在酸性条件下用铁粉还原得到3-氯-4-氟苯胺。
3. 通过缩合反应引入哌嗪基团。
4. 最终环合成诺氟沙星。

安全性

• 急性毒性：静脉注射大鼠LD50 >245 mg/kg，口服小鼠LD50为4000mg/kg；
• 可燃性危险特性：可燃，燃烧时会释放有毒的氮氧化物和氟化物烟雾。

注意事项

诺氟沙星虽然有效，但使用过程中应注意其潜在的不良反应，特别是对肌腱的影响。长期或大剂量使用可能会引起肌腱炎、肌腱断裂等严重副作用，尤其在老年人中更为明显。因此，在临床应用时应严格按照医嘱进行。

总的来说，诺氟沙星是一种非常重要的抗菌药物，在临床上有着广泛的应用。但由于其潜在的毒性和副作用，必须谨慎使用并遵循医生指导。

反应信息

• 作为反应物：
  描述：

  诺氟沙星 在 吡啶 作用下， 以 氯仿 、 水 、 氯甲酸氯甲酯 为溶剂， 生成 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-<4'-<(chloromethoxy)carbonyl>-1'-piperazinyl>quinoline-3-carboxylic acid
  参考文献：
  名称：

  (Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties

  摘要：

  这项发明涉及新型（酰氧烷氧基）羰基衍生物，作为具有主要或次要胺基团的药物中的生物可逆前药基团。水解酶被用来触发碳酸酯前药基团的母体胺药物的再生。该案例还包括药物组合物、治疗方法和工艺要求。

  公开号：

  US04760057A1
• 作为产物：
  描述：

  7-(4-(tert-butoxycarbonyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以68.9%的产率得到诺氟沙星
  参考文献：
  名称：

  [EN] ANTIBIOTIC RESISTANCE BREAKERS
  [FR] AGENTS DE RUPTURE DE RÉSISTANCE AUX ANTIBIOTIQUES

  摘要：

  该发明涉及公式（A1）的抗生素化合物及其药学上可接受的盐、溶剂化合物、互变异构体和它们的组合，其中X和L是可选的连接物，RA或R1中的一个包括Ar1，其中Ar1是一种抗生素耐药性破坏基团，包括可选择取代的C6-10芳基，C7-13芳基烷基，C5-10杂芳基，C6-13杂芳基烷基，C5-10杂环烷基，C6-13杂环烷基，C3-10碳环烷基，C4-13碳环烷基，-C(=NR')-NR'R''或–CH2- CH=CH2基团；在将该化合物用于细菌感染后，该基团减少或预防外流。该发明还公开了包括公式（A1）化合物的药物组合物以及将这些化合物用作药物的用途，特别是用于治疗细菌感染，如耐药性细菌感染。

  公开号：

  WO2018220365A1
• 作为试剂：
  描述：

  咪唑 、 3-碘噻吩 在 诺氟沙星 、 copper(I) bromide 、 sodium hydroxide 作用下， 以 二甲基亚砜 为溶剂， 反应 24.0h， 以53%的产率得到1-(thiophen-3-yl)-1H-imidazole
  参考文献：
  名称：

  商业药物诺氟沙星作为咪唑与芳基卤化物在铜催化的N-芳基化反应中的新型配体

  摘要：

  诺氟沙星被用作咪唑和卤代芳基化合物的CuBr催化的C-N偶联反应的有效配体。该方案具有良好的官能团相容性，允许许多芳基卤化物与咪唑反应形成所需产物，收率高至极佳。

  DOI：

  10.1002/aoc.5195

文献信息

• [EN] DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE<br/>[FR] DÉRIVÉS DE TOXINES D'AMANITES ET LEUR CONJUGAISON À UNE MOLÉCULE DE LIAISON CELLULAIRE
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2017046658A1

  公开（公告）日：2017-03-23

  Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.

  Amernita毒素的衍生物的化学式（I），其中，化学式（a）中的R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、X、L、m、n和Q在此处被定义。这些衍生物的制备。这些衍生物在靶向治疗癌症、自身免疫性疾病和传染病中的治疗用途。
• [EN] A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS<br/>[FR] CONJUGUÉ D'UN AGENT CYTOTOXIQUE À UNE MOLÉCULE DE LIAISON CELLULAIRE AVEC DES LIEURS RAMIFIÉS
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2020257998A1

  公开（公告）日：2020-12-30

  Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.

  提供了一种将细胞毒性药物与一个侧链连接分子结合的共轭物。它提供了制备细胞毒性分子与细胞结合配体的共轭物的侧链连接方法，以及在靶向治疗癌症、感染和免疫性疾病中使用该共轭物的方法。
• [EN] CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES<br/>[FR] DÉRIVÉ DE DIMÈRE DE PYRROLOBENZODIAZÉPINE RÉTICULÉ (PBD) ET SES CONJUGUÉS
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2020006722A1

  公开（公告）日：2020-01-09

  A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

  一种新型的交联细胞毒剂，吡咯苯并二氮杂环二聚体（PBD）衍生物，以及它们与细胞结合分子的结合物，一种制备这些结合物的方法以及这些结合物的治疗用途。
• CYCLOPROPYLAMINES AS LSD1 INHIBITORS
  申请人：Incyte Corporation

  公开号：US20150225379A1

  公开（公告）日：2015-08-13

  The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

  本发明涉及环丙胺衍生物，这些衍生物是LSD1抑制剂，可用于治疗癌症等疾病。
• [EN] ANTIBACTERIAL COMPOUNDS<br/>[FR] COMPOSÉS ANTIBACTÉRIENS
  申请人：MASSACHUSETTS GEN HOSPITAL

  公开号：WO2019199979A1

  公开（公告）日：2019-10-17

  The present application provides compounds of formula: Methods of using these compounds for killing bacterial growth and treating bacterial infections are also provided.

  本申请提供了以下化合物的公式：还提供了使用这些化合物杀灭细菌生长和治疗细菌感染的方法。

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